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Updated: Jan 25, 2026

Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors
Published on: April 9, 2014
Pyrimidine 2,4-Diones in the Design of New HIV RT Inhibitors
Roberto Romeo1, Daniela Iannazzo2, Lucia Veltri3
1Dipartimento di Scienze chimiche, biologiche, farmaceutiche ed ambientali, Università di Messina, Via S.S. Annunziata, 98168 Messina, Italy. robromeo@unime.it.
Abstract:
The pyrimidine nucleus is a versatile core in the development of antiretroviral agents. On this basis, a series of pyrimidine-2,4-diones linked to an isoxazolidine nucleus have been synthesized and tested as nucleoside analogs, endowed with potential anti-HIV (human immunodeficiency virus) activity. Compounds 6a-c, characterized by the presence of an ethereal group at C-3, show HIV reverse transcriptase (RT) inhibitor activity in the nanomolar range as well as HIV-infection inhibitor activity in the low micromolar with no toxicity. In the same context, compound 7b shows only a negligible inhibition of RT HIV.
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